HIV-1 protease inhibitors containing a novel C2 symmetrical hydroxyalkylgem-diamino core structure

Two series of peptidomimetics containing a novel C₂ symmetrical hydroxyalkylgem-diamino core structure were prepared, from amino acid starting materials, and evaluated as inhibitors of HIV-1 protease (HIV-1 Pr). 1, 1-Diamino-3-hydroxypropane (gHse) derivatives showed weak inhibitory potency (IC₅₀> 10 μM). In the 1, 1-diamino-2-hydroxyethane (gSer) series, a compound containing P1/P1’benzyl and P2/P2’Fmoc substitueras, displayed a significant HIV-1 Pr inhibition (IC₅₀= 440 nM). © Munksgaard 1997.